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Current Molecular Pharmacology

Maryam Naserian, Elham Ramazani, Mehrdad Iranshahi, Zahra Tayarani-Najaran
BACKGROUND: Besides the first-line medication for the treatment of type 2 diabetes, the growth inhibitory activity of metformin alone or in combination of conventional chemotherapeutics has been addressed on a panel of cell lines. In this study, we investigated the cytotoxicity and apoptosis of the metformin alone and in combination with dacarbazine in Raji and Ramos lymphoma cell lines. METHODS: Cell viability and apoptosis measured using resazurin assay, flow cytometry of PI stained cells and western blot analysis...
August 30, 2018: Current Molecular Pharmacology
Seyede Hadis Momeni Hasan Abadi, Alireza Shirazi, Ali Mohammad Alizadeh, Vahid Changizi, Masoud Najafi, Solmaz Khalighfard
PURPOSE: Radiation causes damage to irradiated tissues and also tissues that do not receive direct irradiation through a phenomenon called bystander effects. Melatonin as a potent antioxidant and anti-inflammatory agent is known for protection of normal tissues against ionizing irradiation. In addition, some studies have suggested that Melatonin may have some anti-cancer properties. Although the complete mechanisms remain unknown, it can act via immunomodulatory effects. The aim of this study was to evaluate the effect of pretreatment with melatonin on oxidative damage caused by direct irradiation and bystander effects on the lung and heart tissue after xenograft mice colon cancer irradiation in Balb/c mice...
August 30, 2018: Current Molecular Pharmacology
Jagdish K Sahu, Arun K Mishra
BACKGROUND: The brain is a vital part of central nervous system (CNS), characterized by the presence of soft tissue in its internal structure which protects itself from external injury. Research on the design of drugs for CNS disorders is in progress and up to date information is required for further investigation. OBJECTIVE: The present paper is written with objective to compile all the available data and information on CNS disorders and drugs. CNS acting drugs are important to consider due to their active role in the treatment of CNS disorders...
August 20, 2018: Current Molecular Pharmacology
Suhang Hua, Yongxing Zhang
OBJECTIVE: To explore the mechanism by which lobaplatin, as monotherapy and in combination with paclitaxel, inhibits the proliferation of human gastric cancer SGC-7901 cells. METHODS: After treatment, the MTT assay was used to assess cell viability; cell cycle distribution was evaluated flow-cytometrically. Western blot was used to quantitate cyclin D1, E1, B1, and Cdk2/4 protein levels. RESULTS: Lobaplatin and paclitaxel inhibited SGC-7901 cell growth in a concentration and time-dependent manner, with IC25 values at 48h of 1...
August 12, 2018: Current Molecular Pharmacology
Peyman Amini, Hanifeh Mirtavoos-Mahyari, Elahe Motevaseli, Dheyauldeen Shabeeb, Ahmed Eleojo Musa, Mohsen Cheki, Bagher Farhood, Rasoul Yahyapour, Alireza Shirazi, Nouraddin Abdi Goushbolagh, Masoud Najafi
BACKGROUND: Melatonin is a natural body product that has shown potent antioxidant property against various toxic agents. For more than two decades, the abilities of melatonin as a potent radioprotector against toxic effects of ionizing radiation (IR) has been proved. However, in recent years, several studies have been conducted to illustrate how melatonin protects normal cells against IR. Studies proposed that melatonin is able to directly neutralize free radicals produced by IR, leading to the production of some low toxic products...
August 2, 2018: Current Molecular Pharmacology
Ana Carolina Antunes Naime, Jessica Oliveira Frade Ganaes, Maria Elisa Lopes-Pires
OBJECTIVE: Sepsis, a serious and life threatening complication arising from infection caused by lipopolysaccharide, is a complex inflammatory syndrome, and one of the main causes of death in intensive care units (ICU). It is characterized as an over-response of pro-coagulant agents promotes coagulopathy and thrombus formation, resulting in disseminated intravascular coagulation (DIC). Furthermore, it can cause multiple organ dysfunction and hypotension (septic shock) resulting in death...
June 19, 2018: Current Molecular Pharmacology
Rasoul Yahyapour, Dheyauldeen Shabeeb, Mohsen Cheki, Ahmed Eleojo Musa, Bagher Farhood, Abolhasan Rezaeyan, Peyman Amini, Hengameh Fallah, Masoud Najafi
BACKGROUND: Nowadays, ionizing radiations are used for various medical and terroristic aims. These purposes involve exposure to ionizing radiations. Hence, people are at risk for acute or late effects. Annually, millions of cancer patients undergo radiotherapy during their course of treatment. Also, some radiological or nuclear events in recent years pose a threat to people, hence the need for radiation mitigation strategies. Amifostine, the first FDA approved radioprotector, has shown some toxicities that limit its usage and efficiency...
June 19, 2018: Current Molecular Pharmacology
Rhiannon E Roberts, Geetha L Elumalai, Maurice B Hallett
BACKGROUND AND OBJECTIVE: Ezrin links the cortical cytoskeleton to the plasma membrane and plays a role in regulating cell shape change. Recently NSC668394 has been shown to inhibit a key step for its activity, i.e. phosphorylation at threonine 567. In neutrophils, another key regulatory step is the Ca2+-mediated cleavage of ezrin by calpain. METHODS: In this paper we use NSC668394 as a pharmacological inhibitor to investigate the interplay between these two steps in regulating neutrophil shape change...
May 15, 2018: Current Molecular Pharmacology
Keiji Tabuchi, Akira Hara
BACKGROUND AND OBJECTIVE: Sphingolipid metabolites, including ceramide, sphingosine, and their phosphorylates (ceramide-1-phosphonate [C1P] and sphingosine-1-phosphate [S1P]), regulate diverse cellular processes including apoptosis, the cell cycle, and cellular differentiation. Recent studies have shown that these sphingolipid metabolites are generated in response to ototoxic agents and play important roles in determining the fate of cochlear hair cells in ototoxic injury. METHODS: This review summarizes the current knowledge on the roles of sphingolipid mediators in cochlear ototoxicity...
May 15, 2018: Current Molecular Pharmacology
Andy Awad, Pamela El Khoury, Brigitte Wex, Roy A Khalaf
BACKGROUND: Candida albicans is present as part of the normal gut flora and detected in the oral cavities and GI tracts of around fifty percent of adults. Benign colonization can turn pathogenic causing a variety of mild to severe infections. In a pathogen, the cell wall and cell surface proteins are major antigenic determinants and drug targets as they are the primary structures that contact the host. Cell surface proteins perform a variety of functions necessary for virulence such as adhesion, host degradation, resistance to oxidative stress, and drug resistance...
2018: Current Molecular Pharmacology
Michaila Michalatou, Maria Eleni Androutsou, Markos Antonopoulos, Demetrios V Vlahakos, George Agelis, Anthony Zulli, Tawar Qaradakhi, Kathleen Mikkelsen, Vasso Apostolopoulos, John Matsoukas
BACKGROUND: The Renin Angiotensin System (RAS) is pharmacologically targeted to reduce blood pressure, and patient compliance to oral medications is a clinical issue. The mechanisms of action of angiotensin receptor blockers (ARBs) in reducing blood pressure are not well understood and are purported to be via a reduction of angiotensin II signaling. OBJECTIVE: We aimed to develop a transdermal delivery method for ARBs (losartan potassium and valsartan) and to determine if ARBs reveal a vasodilatory effect of the novel RAS peptide, alamandine...
2018: Current Molecular Pharmacology
Shivani Verma, Saurabh Sharma
BACKGROUND: Tyrosine-protein phosphatase is an enzyme that functions in a unit with tyrosine kinases to regulate signaling pathways. Several members of the PTP family link to human disease predisposition such as PTP1B, SH2, DEP1, and inhibition of these enzymes may represent an effective palliative therapy. OBJECTIVE: This review aims to summarize the rapidly developing role of the PTPs in various physiological and pathological states. RESULTS: Pharmacological inhibition of protein tyrosine phosphatase has been found to reduce endothelial dysfunction in different cardiovascular diseases related to metabolic disorders and it can be helpful for the management of other brain disorders associated with perhaps even in normal, agerelated cognitive decline...
2018: Current Molecular Pharmacology
Mohsen Cheki, Rasoul Yahyapour, Bagher Farhood, Abolhassan Rezaeyan, Dheyauldeen Shabeeb, Peyman Amini, Saeed Rezapoor, Masoud Najafi
BACKGROUND: Each year, millions of people die from cancer. Radiotherapy is one of the main treatment strategies for cancer patients. Despite the beneficial roles of treatment with radiation, several side effects may threaten normal tissues of patients in the years after treatment. DISCUSSION: Moreover, high incidences of second primary cancers may reduce therapeutic ratio of radiotherapy. The search for appropriate targets of radiosensitization of tumor cells as well as radioprotection of normal tissues is one of the most interesting aims in radiobiology...
2018: Current Molecular Pharmacology
Nabeela K Dulull, Daniel A Dias, Thilini R Thrimawithana, Faith A A Kwa
BACKGROUND: In age-related macular degeneration, oxidative damage and abnormal neovascularization in the retina are caused by the upregulation of vascular endothelium growth factor and reduced expression of Glutathione-S-transferase genes. Current treatments are only palliative. Compounds from cruciferous vegetables (e.g. L-Sulforaphane) have been found to restore normal gene expression levels in diseases including cancer via the activity of histone deacetylases and DNA methyltransferases, thus retarding disease progression...
2018: Current Molecular Pharmacology
George Liapakis
No abstract text is available yet for this article.
2018: Current Molecular Pharmacology
Michael Kahn
No abstract text is available yet for this article.
2018: Current Molecular Pharmacology
Jessica Felton, Shien Hu, Jean-Pierre Raufman
BACKGROUND: Expression and activation of subtype-3 muscarinic receptors (M3R) plays an important role in the progression of colorectal neoplasia. METHOD: Herein, we describe the role of muscarinic receptors in colon cancer, focusing specifically on M3R, illustrate how M3R over-expression and activation of post-receptor signaling pathways potentiates tumor progression, and explore the efficacy and safety of a variety of therapeutic approaches that can target the molecules involved...
2018: Current Molecular Pharmacology
Rasoul Yahyapour, Peyman Amini, Saeed Rezapoor, Abolhasan Rezaeyan, Bagher Farhood, Mohsen Cheki, Hengameh Fallah, Masoud Najafi
BACKGROUND: Inflammation is the response of the immune system that guards the body against several harmful stimuli in normal conditions. However, in response to ionizing radiation that leads to a massive cell death and DNA aberrations, this phenomenon causes various side effects in normal tissues. Inflammation is involved in various side effects such as gastrointestinal toxicity, mucositis, skin reactions, nervous system damage, pneumonitis, fibrosis and so on. DISCUSSION: Observations have proposed that inflammatory mediators are involved in the toxic effect of ionizing radiation on non-irradiated cells via a phenomenon named bystander effect...
2018: Current Molecular Pharmacology
Maria L Motti, Stefania D Angelo, Rosaria Meccariello
BACKGROUND: MicroRNAs (miRNAs) are small non-coding RNAs able to regulate gene expression at multiple levels. They are detected in tissues, blood, and other body fluids with high stability and have a recognized role in maintaining of tissue homeostasis. Aberrant expression profile of miRNAs has been observed in several diseases, primarily cancer. As a consequence, the analysis of miRNA signature has recognized diagnostic and prognostic role in human diseases, and the development of miRNA-based therapies is currently under investigation...
2018: Current Molecular Pharmacology
Pricila Pfluger, Gabriela Gregory Regner, Vanessa Rodrigues Coelho, Lucas Lima da Silva, Leopoldo Nascimento, Cassiana Macagnan Viau, Regis Adriel Zanette, Cleonice Hoffmann, Jaqueline Nascimento Picada, Jenifer Saffi, Patricia Pereira
BACKGROUND AND OBJECTIVE: Gamma-decanolactone (GD) is a monoterpene effective against seizures induced by pentylenetetrazole. The mechanism of action of GD is likely to be via glutamate antagonism. GD also inhibits intracellular reactive oxygen species (ROS) generation and the lipopolysaccharide-induced expression of inducible nitric oxide synthase (iNOS) and tumor necrosis factor-alpha (TNF-α) in vitro. Considering the neuropharmacological profile of GD studied so far, we investigated the effect of intraperitoneal administration of GD 100 and 300 mg/kg on pilocarpine (PIL)-induced status epilepticus (SE) in mice...
2018: Current Molecular Pharmacology
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